以香草醛和取代扁桃酸为原料,经多步反应合成了N-取代苯乙基扁桃酰胺,在对甲苯磺酸催化下,和醛脱水关环,得到一系列新颖的3-取代苯乙基-5-芳基噁唑4-酮类化合物和N-扁桃酰四氢异喹啉类化合物.所有化合物通过红外光谱、核磁共振氢谱、元素分析和高分辨质谱对其结构进行表征,并对其构效关系进行了讨论.
Mandipropamid is the first mandelamide fungicide on the market. Cyclizing open structures in a given structure represents one of the useful methods in the search for biologically active conformations. A series of novel 3-substituentphenethyl-5-aryloxazolidin-4-ones, the ring-closed analogues of mandipropamid, were obtained from the 2-hydroxy-N-( substitutedphenethyl )-2-arylacetamide and aldehydes by refluxing in benzene or toluene with catalytic amount of p-toluenesulphonic acid. Their structures were identified by means of elemental analysis, IR, ^1H NMR and MS spectra. And their structure-activity relationships were discussed.